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Pharmaceutical composition for treatment of osteoarthritis

Inactive Publication Date: 2013-03-21
NAT DEFENSE MEDICAL CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The technical effect of this patent is to provide a pharmaceutical composition that can treat osteoarthritis by preventing the loss of collagen and proteoglycan, which are caused by TNF (tumor necrosis factor). The composition should also provide symptomatic relief and slow down the degradation of cartilage in osteoarthritis patients.

Problems solved by technology

The degenerative arthritis of the knee joint is likely to get progressively worse as people age.
After a long time, the cartilage at a surface of the knee joint is damaged.
These lead to clinical syndromes of the knee joint such as pain, swelling, disability, having difficulty in squatting and sitting.
However, the steroids have a plenty of common side effects such as upper gastrointestinal bleeding, thinning of the skin, osteoporosis, slower wound healing, etc.
However, glucosamine also has side effects including gastrointestinal discomfort, nausea, diarrhea, etc.
As to the sodium hyaluronate, it's more difficult to secure material and the injection is an invasive procedure.

Method used

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  • Pharmaceutical composition for treatment of osteoarthritis
  • Pharmaceutical composition for treatment of osteoarthritis
  • Pharmaceutical composition for treatment of osteoarthritis

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Embodiment Construction

[0027]In prior arts related to treatment of arthritis, most of them increase production of cartilage matrix, instead of suppressing the degeneration and damage of cartilage matrix. The present invention provides a pharmaceutical composition for treatment of osteoarthritis that focuses on suppression of degeneration and damage of cartilage matrix.

[0028]Refer to FIG. 1, a chemical structure of an embodiment according to the present invention is revealed. As shown in figure, the compound is 2-hydroxy-N-[3-(trifluoromethyl) phenyl]benzamide (hereafter referred to as HS—Cf).

[0029]Refer to FIG. 2, a method for the synthesis of HS—Cf is revealed. As shown in the figure, dissolve 0.276 g (2 mmol) salicylic acid into 10 ml dichloromethane. Then add 0.270 g (2 mmol) 1H-Benzotriazol-1-ol hydrate and 0.270 g (2 mmol) Ethylene dichloride (EDC) into the solution. Next 0.354 ml (2.2 mmol) 3-trifluoromethylaniline is further added into and reacted with the solution for 72 hours. The reacted solutio...

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Abstract

A pharmaceutical composition including 2-hydroxy-N—[3-(trifluoromethyl)phenyl]benzamide and used for treatment of osteoarthritis is revealed. The pharmaceutical composition inhibits tumor necrosis factor (TNF) induced interferon regulatory factor (IRF). The activated IRF stimulates chondrocytes to secret matrix metalloproteinases, inducible nitric oxide synthase (iNOS), aggrecanases, etc. This leads to loss of collagen II and further causes degradation of proteoglycan. By suppression of signaling pathways of interferon regulatory factor, symptoms are relieved and osteoarthritis is treated.

Description

BACKGROUND OF THE INVENTION[0001]1. Field of the Invention[0002]The present invention relates to a pharmaceutical composition, especially to a pharmaceutical composition used as potential drug candidates for treatment of osteoarthritis.[0003]2. Descriptions of Related Art[0004]Osteoarthritis is the most common joint disorder, also known as degenerative arthritis. The knee joint is the largest joint in the body and is one of the most easy to get degenerated and damaged joints. The knee joint is covered by a layer of cartilage that is composed of chondrocytes, collagen and proteoglycans secreted by chondrocytes, and water. The cartilage is like a pad between the ends of bones which form joints, acting as a buffer. The degenerative arthritis of the knee joint is likely to get progressively worse as people age. The degenerative arthritis is the result of long-term stresses on a joint. After a long time, the cartilage at a surface of the knee joint is damaged. Moreover, synovial fluid in...

Claims

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Application Information

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IPC IPC(8): C07C235/56
CPCC07C235/56
Inventor HUANG, HSU-SHANLAI, JENN-HAUNGHO, LING-JUNLIU, FENG-CHENG
Owner NAT DEFENSE MEDICAL CENT
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